5-芳基-6-甲基-4,5-二氢哒嗪-3(2H)酮及相关的5-芳基-6-甲基哒嗪-3(2H)酮的合成与药理研究
Synthesis and pharmacological study of 5-aryl-6-methyl-4,5-dihydro-pyridazin-3(2H)ones and related 5-aryl-6-methyl-pyridazin-3(2H)ones.
作者信息
Pinna G A, Curzu M M, Barlocco D, Cignarella G, Cavalletti E, Germini M, Berger K
机构信息
Istituto di Chimica Farmaceutica, Facoltà di Farmacia, Università di Sassari, Italy.
出版信息
Farmaco Sci. 1988 Jun;43(6):539-49.
New 5-aryl-6-methyl-4,5-dihydropyridazin-3(2H)ones (III) and related 5-aryl-6-methyl-pyridazin-3(2H)ones (IV) were synthesized in order to evaluate their pharmacological profile in comparison with that of the known class of antihypertensive and platelet aggregation inhibitors 5-methyl-6-aryl-4,5-dihydropyridazin 3(2H)ones (I). Though none of the tested derivatives was found to possess the antihypertensive potency of the reference compounds, some of them displayed significant antithrombotic and antiulcer properties. In particular, 5(p. acetylaminophenyl)-6-methyl-pyridazin-3-one (IV c) was found highly effective (ED50 = 1.2 mg/kg) in inhibiting indomethacin-induced ulcers.
合成了新型5-芳基-6-甲基-4,5-二氢哒嗪-3(2H)酮（III）及相关的5-芳基-6-甲基哒嗪-3(2H)酮（IV），以便与已知的抗高血压和血小板聚集抑制剂5-甲基-6-芳基-4,5-二氢哒嗪-3(2H)酮（I）类药物相比，评估它们的药理学特性。尽管未发现所测试的衍生物具有参考化合物的抗高血压效力，但其中一些显示出显著的抗血栓形成和抗溃疡特性。特别是，发现5-(对乙酰氨基酚苯基)-6-甲基哒嗪-3-酮（IV c）在抑制吲哚美辛诱导的溃疡方面非常有效（半数有效剂量=1.2毫克/千克）。
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